Compounds having selective partial agonist activity at the 5-HT1A receptor have established a presence in the marketplace as effective anxiolytic agents (e.g., buspirone, Buspar®, U.S. Pat. No. 3,717,634). 5-HT1A agonists and antagonists may find use in the treatment of several diseases such as anxiety, depression, schizophrenia, cognitive deficits resulting from neurodegenerative diseases like Alzheimer's Disease, nausea and vomiting, and in the treatment of prostate cancer (for recent references, see: K. Rasmussen and V. P. Rocco, Recent Progress in Serotonin (5-HT)1A Receptor Modulators, in Annual Reports in Medicinal Chemistry, Volume 30, J. A. Bristol, ed., pp. 1–9 (1995)).
Compounds which are active at the 5HT1A receptor have been disclosed in U.S. Pat. Nos. 4,873,331, 4,882,432, 4,988,814, 5,340,812, 5,486,518, and 5,519,025, in European Patent 395,313, and in PCT applications published as WO 00/52002, WO 00/35874, WO 00/51999, and WO 99/65887.